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Vol. 54, Issue 2, 203-218, June 2002

International Union of Pharmacology. XXVIII. Proteinase-Activated Receptors

Morley D. Hollenberg and Steven J. Compton1

Endocrine, Mucosal Inflammation, Smooth Muscle and Cancer Biology Research Groups, Department of Pharmacology and Therapeutics and Department of Medicine, University of Calgary, Faculty of Medicine, Calgary, Alberta, Canada

I. Introduction
II. Nomenclature and Use of the Proteinase-Activated Receptor Designation
III. Receptor Subtypes
    A. Defining Proteinase-Activated Receptor Subtypes Using Enzyme and Peptide Agonists
    B. Receptor Antagonists and Receptor Subtypes
    C. Molecular Definition of Receptor Subtypes
IV. Molecular Aspects of Proteinase-Activated Receptor Activation
    A. The Tethered Ligand Mechanism
    B. Structure-Activity Relationships for Receptor Activation by the Tethered Ligand Sequences
    C. Receptor Domains Involved in Ligand Activation
    D. Signaling, Desensitization, and Receptor Internalization
    E. Receptor Activation and Proteinase Susceptibility: What Are the Endogenous Proteinase-Activated Receptor Regulators?
V. Physiological Roles of Proteinase-Activated Receptors
    A. Thrombin Targets: Proteinase-Activated Receptors 1, 3, and 4
    B. Proteinase-Activated Receptor 2, a Trypsin Target
VI. Future Issues and Conclusions
Acknowledgments
References

Proteinase-activated receptors (PARs) represent a unique subclass of G-protein-coupled receptors of which four family members have now been cloned from a number of species. The novel mechanism of receptor activation involves the proteolytic unmasking of a cryptic N-terminal receptor sequence that, remaining tethered, binds to and triggers receptor function. In addition, short (five to six amino acids) synthetic peptides, based on the proteolytically revealed motif, can activate PARs without the unmasking of the tethered ligand. This article summarizes the experiments leading to the pharmacological characterization and cloning of the four PAR family members and provides a rationale for their designation by the acronym "PAR". The ability to distinguish among the PARs pharmacologically 1) with selective proteinase activators, 2) with receptor-selective peptide agonists, and 3) with peptide and nonpeptide antagonists is discussed, as are the molecular mechanisms of receptor activation and desensitization/internalization. Finally, the potential physiological roles of the PARs, which are widely distributed in many organs in the settings of tissue injury, repair, and remodeling, including embryogenesis and oncogenesis are discussed, and the newly appreciated roles of proteinases as signaling molecules that can act as either functional agonists or antagonists are highlighted.

1 Present address: Academic Dept. of Medicine, University of Hull, Castle Hill Hospital, Castle Road, Cottingham, Hull HU16 5JQ, UK.

0031-6997/02/5402-0203$03.00/0
PHARMACOLOGICAL REVIEWS
Copyright © 2002 by The American Society for Pharmacology and Experimental Therapeutics


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